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Exploring Heterocycle-Spermine Conjugates as Modulators of Oncogenic microRNAs Biogenesis

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journal contribution
posted on 04.12.2018, 09:14 by Cécile Becquart, Myriame Le Roch, Stéphane Azoulay, Philippe Uriac, Audrey Di Giorgio, Maria Duca
Targeting biologically relevant noncoding RNAs using small molecules is currently one of the major challenges of medicinal chemistry but holds a great potential for future therapeutic applications. In this context, oncogenic microRNAs represent a particularly promising target, and various examples of RNA binders have been reported as inhibitors of the biogenesis of these microRNAs. Here, we report the biochemical evaluation and molecular docking studies of five heterocycle-spermine conjugates revealing that a structure-based design of efficient and especially selective inhibitors can be performed based on the secondary and tertiary configuration of the targeted RNA.